LIDOCAINE HYDROCHLORIDE instructions for use, description of the drug LIDOCAINE HYDROCHLORIDE: contraindications, side effects, dosages, composition - solution for injection in the lek reference book

Description of the drug LIDOCAINE HYDROCHLORIDE

When used simultaneously with barbiturates (including phenobarbital), it is possible to increase the metabolism of lidocaine in the liver, reduce the concentration in the blood plasma and, as a result, reduce its therapeutic effectiveness.

When used simultaneously with beta-blockers (including propranolol, nadolol), the effects of lidocaine (including toxic ones) may be enhanced, apparently due to a slowdown in its metabolism in the liver.

When used simultaneously with MAO inhibitors, the local anesthetic effect of lidocaine may be enhanced.

When used simultaneously with drugs that block neuromuscular transmission (including suxamethonium chloride), the effect of drugs that block neuromuscular transmission may be enhanced.

When used simultaneously with hypnotics and sedatives, the inhibitory effect on the central nervous system may be enhanced; with ajmaline, quinidine - possible increased cardiodepressive effect; with amiodarone - cases of seizures and SSSS have been described.

When used simultaneously with hexenal, sodium thiopental (iv), respiratory depression is possible.

When used simultaneously with mexiletine, the toxicity of lidocaine increases; with midazolam - a moderate decrease in the concentration of lidocaine in the blood plasma; with morphine - enhances the analgesic effect of morphine.

When used simultaneously with prenylamine, there is a risk of developing ventricular arrhythmias.

Cases of agitation and hallucinations have been described when used simultaneously with procainamide.

When used simultaneously with propafenone, the duration and severity of side effects from the central nervous system may increase.

It is believed that under the influence of rifampicin, a decrease in the concentration of lidocaine in the blood plasma is possible.

With simultaneous intravenous infusion of lidocaine and phenytoin, side effects of central origin may increase; a case of sinoatrial block due to the additive cardiodepressive effect of lidocaine and phenytoin is described.

In patients receiving phenytoin as an anticonvulsant, a decrease in the concentration of lidocaine in the blood plasma is possible, which is due to the induction of microsomal liver enzymes under the influence of phenytoin.

When used simultaneously with cimetidine, the clearance of lidocaine moderately decreases and its concentration in the blood plasma increases, and there is a risk of increased side effects of lidocaine.

LIDOCAINE

Directions for use and doses

The amount of solution and the total dose of lidocaine depends on the type of anesthesia, the nature and duration of the surgical intervention.
Method of diluting 20 mg/ml (2%) lidocaine solution to obtain a solution of the required concentration:

To prepare a 10 mg/ml (1%) lidocaine solution, you need to take 1 part of a 20 mg/ml lidocaine solution and 1 part of water for injection, i.e. mix 2 ml of 20 mg/ml lidocaine solution with 2 ml of water for injection (for a 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 5 ml of water for injection (for a 5 ml ampoule).

To prepare a 5 mg/ml (0.5%) lidocaine solution, you need to take 1 part of a 20 mg/ml lidocaine solution and 3 parts of water for injection, i.e. mix 2 ml of 20 mg/ml lidocaine solution with 6 ml of water for injection (for a 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 15 ml of water for injection (for a 5 ml ampoule).

To prepare a 2.5 mg/ml (0.25%) lidocaine solution, you need to take 1 part of a 20 mg/ml lidocaine solution and 7 parts of water for injection, i.e. mix 2 ml of a 20 mg/ml lidocaine solution with 14 ml of water for injection (for a 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 35 ml of water for injection (for a 5 ml ampoule).

To prepare a 1.25 mg/ml (0.125%) lidocaine solution, you need to take 1 part of a 20 mg/ml lidocaine solution and 15 parts of water for injection, i.e. mix 2 ml of a 20 mg/ml lidocaine solution with 30 ml of water for injection (for a 2 ml ampoule), or mix 5 ml of 20 mg/ml lidocaine solution with 75 ml of water for injection (for a 5 ml ampoule).

For infiltration anesthesia

(intradermal, subcutaneous) 0.125%, 0.25%, 0.5% solutions are used; to achieve infiltration anesthesia, up to 60 ml (5-300 mg) of a 0.5% solution or up to 30 ml of a 1% solution is used.

For conduction anesthesia

(anaesthesia of peripheral nerves, including blockade of nerve plexuses) use 1 and 2% solutions; the maximum total dose is up to 400 mg (40 ml of a 1% solution or 20 ml of a 2% solution). For nerve plexus blockade, 10-20 ml of a 1% solution or 5-10 ml of a 2% solution.

For conduction anesthesia of peripheral nerves

: brachial - 15-20 ml (225-300 mg) 1.5% solution; in dental practice - 1-5 ml (20-100 mg) of 2% solution; blockade of intercostal nerves - 3 ml (30 mg) of 1% solution.

For paracervical anesthesia:

10 ml (100 mg) of 1% solution in each direction, if necessary, re-administration is possible after at least 1.5 hours.

For paravertebral anesthesia

: from 3 to 5 ml (30-50 mg) of 1% solution.
Retrobulbar anesthesia -
3.0-4.0 (60-80 mg) 2% solution.

Parabulbar anesthesia

- 1.0-2.0 (20-40 mg) 2% solution.
Vagosympathetic blockade:
cervical (stellate ganglion) - 5 ml (50 mg) of 1% solution, lumbar - 5-10 ml (50-100 mg) of 1% solution.

Spinal anesthesia

- 3.0-4.0 ml (60-80 mg) 2% solution.

Epidural anesthesia -

to obtain analgesia, 25-30 ml (250-300 mg) of a 1% solution is used; to obtain anesthesia, 15-20 ml (225-300 mg) of a 1.5% solution or 10-15 ml (200-300 mg) of a 2% solution; for thoracic epidural anesthesia - 20-30 ml (200-300 mg) of 1% solution. Continuous administration of anesthetic via a catheter is not recommended; administration of the maximum dose should not be repeated more often than after 90 minutes.

When using caudal anesthesia:

in surgical practice - 15-20 ml (225-300 mg) of a 1.5% solution. Continuous administration of anesthetic via a catheter is not recommended; administration of the maximum dose should not be repeated more often than after 90 minutes. Recommended doses for children with neuromuscular blockade are up to 4.5 mg/ml of a 0.25-1.0% solution.

The maximum dose for children is 4.5 mg/kg, but not more than 100 mg; the maximum dose for adults is no more than 4.5 mg/kg or 300 mg. These doses must be repeated within 24 hours.

The effect of lidocaine can be prolonged by adding a 0.1% epinephrine solution (0.1 ml per 20 ml of lidocaine). In this case, with regional anesthesia, the dose of lidocaine can be increased to 600 mg.

Procedure for working with a polymer ampoule:

1.Take the ampoule and shake it, holding it by the neck.

2. Squeeze the ampoule with your hand, without releasing the drug, and use a rotating motion to turn and separate the valve.

3. Immediately connect the syringe to the ampoule through the resulting hole.

4. Turn the ampoule over and slowly draw its contents into the syringe.

5. Place the needle on the syringe.

Lidocaine, 20 mg/ml, solution for injection, 2 ml, 10 pcs.

When used simultaneously with MAO inhibitors, the local anesthetic effect of lidocaine may be enhanced.

When used simultaneously with drugs that block neuromuscular transmission (including suxamethonium chloride), the effect of drugs that block neuromuscular transmission may be enhanced.

When used simultaneously with hexenal, sodium thiopental (iv), respiratory depression is possible.

When used simultaneously with prenylamine, there is a risk of developing ventricular arrhythmias.

Cases of agitation and hallucinations have been described when used simultaneously with procainamide.

When used simultaneously with propafenone, the duration and severity of side effects from the central nervous system may increase.

It is believed that under the influence of rifampicin, a decrease in the concentration of lidocaine in the blood plasma is possible.

Lidocaine 10% 50ml 38g spray for topical use dosed

pharmachologic effect

Local anesthetic for superficial anesthesia.
The action is due to the blockade of voltage-dependent sodium channels, which prevents the generation of impulses at the endings of sensory nerves and the conduction of pain impulses along nerve fibers. When applied topically, it dilates blood vessels and does not have a local irritating effect. Has an analgesic effect.

The effect develops 1-5 minutes after application to mucous membranes or skin and lasts 30-60 minutes.

Composition and release form Lidocaine 10% 50ml 38g spray for topical use, dosed

Spray - 1 dose/1 bottle:

Active substance: lidocaine 4.6 mg 3.8 g.
Excipients: peppermint leaf oil, propylene glycol, ethanol 96%.

38 g (650 doses) - dark glass bottles with a capacity of 50 ml (1) with a dosing pump with a spray head - cardboard packs.

Description of the dosage form

Spray for topical use dosed in the form of an almost colorless alcohol solution with a characteristic menthol odor.

Characteristic

Acetanilide derivative.

Directions for use and doses

The drug is used locally, externally. The dose depends on the indications and the area of the anesthetized surface.

1 dose of spray, released by pressing the dosing valve, contains 4.8 mg of lidocaine.

To avoid high concentrations of lidocaine in blood plasma, the lowest dose that provides a satisfactory effect should be used. Usually 1-2 sprays are sufficient, although 15-20 sprays or more are used in obstetrics (maximum dose - 40 sprays/70 kg body weight).

Recommended doses for various indications:

Application area	Dose (number of sprays)
Dentistry	1-3
Oral surgery	1-4
Otorhinolaryngology	1-4
Endoscopy	2-3
Obstetrics	15-20
Gynecology	4-5
Dermatology	1-3

The drug can also be applied using a cotton swab soaked in it.

When performing dental procedures and surgeries in children, it is preferable to apply Lidocaine spray using a cotton swab, which avoids the fear of spraying the drug, as well as the tingling sensation (a common side effect).

Pharmacokinetics

Suction

Rapidly absorbed from mucous membranes (especially the pharynx and respiratory tract). The degree of absorption of the drug is determined by the degree of blood supply to the mucous membrane, the total dose of the drug, the localization of the site and the duration of application. After application to the mucous membrane of the upper respiratory tract, it is partially swallowed and inactivated in the gastrointestinal tract. The time to reach Cmax when applied to the mucous membrane of the oral cavity and upper respiratory tract is 10-20 minutes.

Distribution

Protein binding depends on the concentration of the drug and is 60-80% at a drug concentration of 1-4 μg/ml (4.3-17.2 μmol/l). It is distributed quickly (T1/2 phases of distribution - 6-9 minutes), first enters well-supplied tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates the BBB and placental barrier, secreted into breast milk (40% of the concentration in maternal plasma).

Metabolism and excretion

Metabolized in the liver (90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and cleavage of the amide bond with the formation of metabolites that are less active compared to lidocaine (monoethylglycine xylidine and glycine xylidine), T1/2 of which is 2 hours and 10 hours, respectively.

Excreted with bile and kidneys (up to 10% unchanged).

Pharmacokinetics in special groups of patients

In liver diseases, the metabolic rate decreases and ranges from 50% to 10% of the normal value.

In chronic renal failure, accumulation of metabolites is possible.

Indications for use Lidocaine 10% 50ml 38g spray for topical use, dosed

For terminal (superficial) anesthesia of mucous membranes.

In dentistry:

anesthesia of the injection area before local anesthesia;
suturing the mucous membrane;
removal of mobile baby teeth;
removal of tartar;
anesthesia of the gums before fixing a crown or bridge;
in children during surgery for excision of the frenulum of the tongue and opening of salivary gland cysts.

In otorhinolaryngology:

operations on the nasal septum;
carrying out electrocoagulation.

In obstetrics and gynecology:

episiotomy and incision debridement;
removal of seams;
interventions on the vagina and cervix.

For instrumental and endoscopic studies:

insertion of a probe, rectoscopy, intubation, etc.;
X-ray examination (to eliminate nausea and pharyngeal reflex).

In surgery and dermatology:

as an analgesic drug for burns (including sunburn), small wounds (including scratches);
superficial anesthesia of the skin during minor surgical interventions.

Contraindications

Use for tonsillectomy and adenotomy in children under 8 years of age;
hypersensitivity to lidocaine and other components of the drug.

The drug should be used with caution during instrumental studies (rectoscopy) in patients with hemorrhoidal bleeding, local infection in the area of application, trauma to the mucous membrane or skin in the area of application, severe somatic pathology, epilepsy, bradycardia, impaired cardiac conduction, impaired liver function, severe shock, in young children, elderly patients, during pregnancy and lactation.

Application Lidocaine 10% 50ml 38g spray for topical use dosed during pregnancy and breastfeeding

There are no results from controlled clinical studies in pregnant women. If local anesthesia is necessary and there is no safer treatment, lidocaine spray can be used during pregnancy.

Lidocaine is excreted in breast milk, but after topical use in normal therapeutic doses, the amount excreted in milk is too small to cause any harm to a nursing infant.

Use in children

In children under 2 years of age, it is preferable to use the drug by applying it with a swab, which avoids the fear that appears when spraying, as well as the burning sensation.

It should be borne in mind that in children the swallowing reflex occurs much more often than in adults.

Lidocaine in aerosol form is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

special instructions

It is important to prevent lidocaine from entering the respiratory tract (risk of aspiration). Application to the throat requires special attention.

Application to the buccal mucosa is associated with a risk of dysphagia and subsequent aspiration, especially in children. If the sensitivity of the tongue and mucous membrane of the cheeks is impaired, the risk of biting them increases.

Lidocaine is well absorbed through mucous membranes (especially in the trachea) and damaged skin. This should be taken into account, especially when treating large areas of tissue in children.

In cases of using the spray during surgical operations in the pharynx or nasopharynx, it should be taken into account that lidocaine, suppressing the pharyngeal reflex, enters the larynx and trachea and suppresses the cough reflex, which can lead to bronchopneumonia. This is especially important in children, as they are more likely to trigger their swallowing reflex. In this regard, the spray is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

Caution should be exercised when applying lidocaine to damaged mucous membranes and/or infected areas.

The drug should be used with caution in patients with epilepsy, as well as bradycardia, cardiac conduction disorders, liver dysfunction and severe shock, especially when significant amounts of the drug can be expected to be absorbed when large areas of tissue are treated with high doses.

The drug in lower doses should be used in weakened and elderly patients, in acute diseases, as well as in children - in accordance with age and general condition.

In children under 2 years of age, it is recommended to apply Lidocaine spray with a cotton swab dipped in the drug.

During application of the drug, the bottle should be kept as vertical as possible. The spray should not get into your eyes. Do not open the bottle or heat it.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: increased sweating, pale skin, dizziness, headache, blurred vision, ringing in the ears, diplopia, decreased blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, convulsions, methemoglobinemia, cardiac arrest.

Treatment: when the first signs of intoxication appear (dizziness, nausea, vomiting, euphoria), further administration is stopped and the patient is transferred to a horizontal position; oxygen inhalation is prescribed; for convulsions - 10 mg diazepam intravenously; for bradycardia - m-anticholinergic blockers (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

Side effects Lidocaine 10% 50ml 38g spray for topical use dosed

Local reactions: a slight tingling sensation that disappears as the anesthetic effect develops (within 1 minute); Transient erythema, swelling and sensory disturbances may occur.

Allergic reactions: very rarely - urticaria, angioedema, bronchospasm; in exceptional cases - anaphylactic shock. The use of the drug should be stopped immediately if any allergic reaction occurs.

The frequency of systemic effects after topical use of the drug is extremely low, because Only a very small amount of the active substance can enter the bloodstream.

From the side of the central nervous system: very rarely - nervous excitement, systemic dizziness, insomnia, loss of consciousness and respiratory paralysis.

From the cardiovascular system: decreased blood pressure, depression of myocardial function, bradycardia, cardiac arrest.

Drug interactions

Cimetidine and propranolol reduce the hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation and decreased hepatic blood flow) and increase the risk of toxic effects (including stunned state, drowsiness, bradycardia, paresthesia, etc.).

Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce effectiveness (an increase in dose may be required).

When prescribed with ajmaline, phenytoin, verapamil, quinidine, amiodarone, the negative inotropic effect may be enhanced. Co-administration with beta-blockers increases the risk of bradycardia.

Curare-like drugs enhance muscle relaxation.

Procainamide increases the risk of developing central nervous system excitation and hallucinations.

With the simultaneous administration of lidocaine and hypnotics and sedatives, their inhibitory effect on the central nervous system may be enhanced.

With intravenous administration of hexobarbital or sodium thiopental against the background of the action of lidocaine, respiratory depression is possible.

Under the influence of MAO inhibitors, the local anesthetic effect of lidocaine may be enhanced.

With the simultaneous use of lidocaine and polymyxin B, an increased inhibitory effect on neuromuscular transmission is possible, so in this case it is necessary to monitor the patient's respiratory function.